Dapagliflozin
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| Systematic (IUPAC) name | |
| (2S,3R,4R,5S,6R)-2-[4-chloro-3- | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Routes | Oral |
| Identifiers | |
| CAS number | 461432-26-8  |
| ATC code | A10BX09 |
| PubChem | CID 9887712 |
| ChemSpider | 8063384  |
| UNII | 1ULL0QJ8UC |
| ChEMBL | CHEMBL429910 |
| Synonyms | BMS-512148 |
| Chemical data | |
| Formula | C21H25ClO6 |
| Mol. mass | 408.873 g/mol |
| SMILES | eMolecules & PubChem |
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Dapagliflozin (rINN/USAN)[1] is an experimental drug being studied by Bristol-Myers Squibb in partnership with AstraZeneca as a potential treatment for type 1[1] and 2 diabetes. Although dapagliflozin's method of action would operate on either type of diabetes or other conditions resulting in hyperglycemia, the current clinical trials specifically exclude participants with Type 1 diabetes.[2][3]
In July 2011 an FDA committee recommended against approval until more data was available.[4] The Prescription Drug User Fee Act (PDUFA) date for dapagliflozin for the treatment of Type 2 diabetes was extended three months by the FDA to January 28, 2012.[citation needed]
[edit] Method of action
Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.[5]
[edit] Selectivity
The IC50 for SGLT2 is less than one thousandth of the IC50 for SGLT1 (1.1 versus 1390 nmol/l), so that the drug does not interfere with the intestinal glucose absorption.[6]
[edit] References
- ^ a b Statement on a nonproprietory name adopted by the USAN council
- ^ Efficacy and Safety of Dapagliflozin, Added to Therapy of Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin, ClinicalTrials.gov, April 2009
- ^ Trial Details for Trial MB102-020, Bristol-Myers Squibb, May 2009
- ^ "FDA panel advises against approval of dapagliflozin". 19 July 2011. http://www.hemonctoday.com/article.aspx?rid=85812.
- ^ Prous Science: Molecule of the Month November 2007
- ^ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009
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